专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4237133A 1,9-Dihydroxyoctahydrophenanthrenes 失效
标题翻译： 1,9-二羟基焦氢氯苯
公开(公告)号：US4237133A
公开(公告)日：1980-12-02
申请号：US78473
申请日：1979-09-24
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/72 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/83 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , C07D295/14 , A61K31/22 , A61K31/535 , C07C101/19
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/72 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2)is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R1是氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH2）p-NR'R“，其中p是0或 1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

2. 发明授权

US4387229A 3-[2-Hydroxy-4-(substituted)phenyl]azacycloalkanols and derivatives thereof 失效
标题翻译： 3- [2-羟基-4-（取代的）苯基]氮杂环烷醇及其衍生物
公开(公告)号：US4387229A
公开(公告)日：1983-06-07
申请号：US353113
申请日：1982-02-26
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07D211/22 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07F9/59 , C07D207/12 , C07D223/02 , C07D225/00
CPC分类号： C07D211/42 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07F9/592
摘要： Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
摘要翻译：氮杂环烷烃及其衍生物，包括不饱和类似物，其各自在3-位上具有2-羟基-4-取代的苯基，其中4-位取代基是可以具有氧原子作为链的一部分的烷基，或可以具有氧原子作为烷基链的一部分的芳烷基，其用于药理和药用目的，其中间体及其制备方法。

3. 发明授权

US4188495A 1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor 失效
标题翻译： 1,9-二羟基八氢菲和其中间体
公开(公告)号：US4188495A
公开(公告)日：1980-02-12
申请号：US851503
申请日：1977-11-14
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C69/017 , A61K31/045 , A61K31/075 , A61K31/12 , A61K31/13 , A61K31/215 , A61K31/395 , A61P1/00 , A61P7/10 , A61P9/12 , A61P25/04 , A61P25/20 , A61P37/06 , C07C35/42 , C07C41/00 , C07C41/22 , C07C41/26 , C07C43/178 , C07C43/196 , C07C43/20 , C07C43/225 , C07C43/23 , C07C45/00 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/59 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/417 , C07C49/587 , C07C49/643 , C07C49/733 , C07C49/737 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/82 , C07C49/83 , C07C67/00 , C07C69/013 , C07C229/06 , C07C313/00 , C07C317/00 , C07C317/18 , C07C317/22 , C07C323/20 , C07C323/22 , C07D211/00 , C07D211/22 , C07D211/32 , C07D213/00 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , A61K31/085
CPC分类号： C07D213/30 , C07C255/00 , C07C323/00 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/59 , C07C45/61 , C07C45/67 , C07C45/673 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO, and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0或1至 4; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

4. 发明授权

US4310529A Intermediates to 1,9-dihydroxyoctahydrophenanthrenes 失效
标题翻译：中间体至1,9-二羟基焦合氢离子
公开(公告)号：US4310529A
公开(公告)日：1982-01-12
申请号：US218712
申请日：1980-12-22
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , A61K31/44 , A61K31/445 , C07D213/55
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0 或1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n - 其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

5. 发明授权

US4268523A 1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor 失效
标题翻译： 1,9-二羟基八氢菲和其中间体
公开(公告)号：US4268523A
公开(公告)日：1981-05-19
申请号：US78476
申请日：1979-09-24
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/83 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , A01N35/00 , C07C49/788
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n - wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R1是氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH2）p-NR'R“，其中p是0或 1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

6. 发明授权

US4391827A 3-(2-Hydroxy-4-(substituted)phenyl)-cycloalkanone and cycloalkanol analgesic agents and intermediates therefor 失效
标题翻译： 3-（2-羟基-4-（取代的）苯基） - 环烷酮和环烷基醇镇痛剂及其中间体
公开(公告)号：US4391827A
公开(公告)日：1983-07-05
申请号：US286809
申请日：1981-07-27
申请人： Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： A61K31/045 , A61K31/085 , C07C37/00 , C07C37/055 , C07C39/17 , C07C39/23 , C07C39/42 , C07C41/26 , C07C41/56 , C07C43/23 , C07C45/28 , C07C45/30 , C07C45/32 , C07C45/38 , C07C45/72 , C07C49/255 , C07C49/747 , C07C49/753 , C07D317/72 , C07F9/117 , A61K31/12 , C07C49/237
CPC分类号： C07D317/72 , C07C37/002 , C07C37/055 , C07C37/0555 , C07C39/17 , C07C39/23 , C07C39/42 , C07C403/02 , C07C41/26 , C07C41/48 , C07C41/56 , C07C43/23 , C07C49/255 , C07C49/747 , C07C49/753 , C07F9/117 , C07C2101/14 , C07C2101/16 , C07C2101/18
摘要： Cycloalkanones, cycloalkanols and unsaturated analogs thereof, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
摘要翻译：环烷烃，环烷醇和其不饱和类似物，其中3位具有2-羟基-4-取代的苯基，其中4位取代基是可以具有氧原子作为链的一部分的烷基，或芳烷基，可以具有氧原子作为烷基链的一部分，其用于药理和药用目的，其中间体及其制备方法。

7. 发明授权

US4332942A 3-(2-Hydroxy-4-(substituted)phenyl)azacycloalkanes as analgesics 失效
标题翻译： 3-（2-羟基-4-（取代的）苯基）氮杂环烷烷作止痛剂
公开(公告)号：US4332942A
公开(公告)日：1982-06-01
申请号：US198742
申请日：1980-10-20
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07D211/22 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07D211/34
CPC分类号： C07D211/46 , C07D211/22 , C07D211/42 , C07D211/44 , C07D211/48 , C07D211/70 , C07D211/74
摘要： Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
摘要翻译：氮杂环烷烃及其衍生物，包括不饱和类似物，其各自在3-位上具有2-羟基-4-取代的苯基，其中4-位取代基是可以具有氧原子作为链的一部分的烷基，或可以具有氧原子作为烷基链的一部分的芳烷基，其用于药理和药用目的，其中间体及其制备方法。

8. 发明授权

US4310669A Intermediates to 1,9-dihydroxyoctahydrophenanthrenes 失效
标题翻译：中间体至1,9-二羟基焦合氢离子
公开(公告)号：US4310669A
公开(公告)日：1982-01-12
申请号：US219319
申请日：1980-12-22
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , C07D213/55 , C07D211/34
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n - wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of Compounds I and II to produce analgesia is also described.
摘要翻译：其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0或1至 4; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生镇痛的方法。

9. 发明授权

US4268692A 1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor 失效
标题翻译： 1,9-二羟基八氢菲和其中间体
公开(公告)号：US4268692A
公开(公告)日：1981-05-19
申请号：US78475
申请日：1979-09-24
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/83 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , C07C49/733 , C07C69/78
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n -wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0或从 1至4; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n - 其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

10. 发明授权

US4263438A 3-[2,4-(Disubstituted)-phenyl]azacycloalkanones as analgesics 失效
标题翻译： 3- [2,4-（二取代） - 苯基]氮杂环烷酮作为镇痛药
公开(公告)号：US4263438A
公开(公告)日：1981-04-21
申请号：US419
申请日：1979-01-02
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07D211/22 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07F9/59
CPC分类号： C07F9/592 , C07D211/22 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74
摘要： Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
摘要翻译：氮杂环烷烃及其衍生物，包括不饱和类似物，其各自在3-位上具有2-羟基-4-取代的苯基，其中4-位取代基是可以具有氧原子作为链的一部分的烷基，或可以具有氧原子作为烷基链的一部分的芳烷基，其用于药理和药用目的，其中间体及其制备方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式